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1

A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors

James P. Guare, John S. Wai, Robert P. Gomez, Neville J. Anthony, Samson M. Jolly, Amanda R. Cortes, Joseph P. Vacca, Peter J. Felock, Kara A. Stillmock, William A. Schleif, Gregory Moyer, Lori J. Gab

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 159 KB

english, 2006

2

New advances in the discovery of thrombin and factor Xa inhibitors

Journal:

Current Opinion in Chemical Biology

Année:

2000

Langue:

english

Fichier:

PDF, 184 KB

english, 2000

3

Design and synthesis of HIV protease inhibitors. Variations of the carboxyterminus of the HIV protease inhibitor L-682,679

DeSolms, S. Jane, Giuliani, Elizabeth A., Guare, James P., Vacca, Joseph P., Sanders, William M., Graham, Samuel L., Wiggins, J. Mark, Darke, Paul L., Sigal, Irving S.

Journal:

Journal of Medicinal Chemistry

Année:

1991

Langue:

english

Fichier:

PDF, 772 KB

english, 1991

4

PL-100, a novel HIV-1 protease inhibitor displaying a high genetic barrier to resistance: An in vitro selection study

Serge Dandache, Craig A. Coburn, Maureen Oliveira, Timothy J. Allison, M. Katharine Holloway, Jinzi J. Wu, Brent R. Stranix, Chandra Panchal, Mark A. Wainberg, Joseph P. Vacca

Journal:

Journal of Medical Virology

Année:

2008

Langue:

english

Fichier:

PDF, 288 KB

english, 2008

5

A potent and orally active HIV-1 integrase inhibitor

Melissa S. Egbertson, H. Marie Moritz, Jeffrey Y. Melamed, Wei Han, Debra S. Perlow, Michelle S. Kuo, Mark Embrey, Joseph P. Vacca, Matthew M. Zrada, Amanda R. Cortes, Audrey Wallace, Yvonne Leonard,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 256 KB

english, 2007

6

A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability

B.Moon Kim, Joseph P. Vacca, James P. Guare, Colleen M. Hanifin, Stuart R. Michelson, PaulL. Darke, Joan A. Zugay, Emilio A. Emini, William Schleif, Jiunn H. Lin, I-Wu Chen, Kari Vastag, Drazen Ostovi

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1994

Langue:

english

Fichier:

PDF, 463 KB

english, 1994

7

Thiophene derivatives as extremely high affinity P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors

B. Moon Kim, James P. Guare, Joseph D. Vacca, Stuart R. Michelson, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William Schleif, Jiunn H. Lin, I.W. Chen, Kari Vastag, Paul S. Anderson, Joel R. Huff

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1995

Langue:

english

Fichier:

PDF, 297 KB

english, 1995

8

Substituted alkylpyridines as P3′ ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles

B. Moon Kim, Colleen M. Hanifin, C. Blair Zartman, Joseph P. Vacca, Stuart R. Michelson, Jiunn H. Lin, I.-W. Chen, Kari Vastag, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William Schleif, Paul S.

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1995

Langue:

english

Fichier:

PDF, 277 KB

english, 1995

9

Cycloalkylpiperazines as HIV-1 protease inhibitors: enhanced oral absorption

B. Moon Kim, Ben E. Evans, Kevin F. Gilbert, Colleen M. Hanifin, Joseph P. Vacca, Stuart R. Michelson, Paul L. Darke, Joan A. Zugay, Emilio A. Emini, William Schleif, Jiunn H. Lin, I.-W. Chen, Kari Va

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1995

Langue:

english

Fichier:

PDF, 287 KB

english, 1995

10

Rational design and synthesis of selective BACE-1 inhibitors

Stephen F. Brady, Satendra Singh, Ming-Chih Crouthamel, M.Katharine Holloway, Craig A. Coburn, Victor M. Garsky, Michael Bogusky, Michael W. Pennington, Joseph P. Vacca, Daria Hazuda, Ming-Tain Lai

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 200 KB

english, 2004

11

Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P1′ group

Philippe G Nantermet, James C Barrow, Stacey R Lindsley, MaryBeth Young, Shi-Shan Mao, Steven Carroll, Carolyn Bailey, Michele Bosserman, Dennis Colussi, Daniel R McMasters, Joseph P Vacca, Harold G S

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 310 KB

english, 2004

12

Low molecular weight thrombin inhibitors with excellent potency, metabolic stability, and oral bioavailability

Matthew M Morrissette, Kenneth J Stauffer, Peter D Williams, Terry A Lyle, Joseph P Vacca, Julie A Krueger, S.Dale Lewis, Bobby J Lucas, Bradley K Wong, Rebecca B White, Cynthia Miller-Stein, Elizabet

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2004

Langue:

english

Fichier:

PDF, 283 KB

english, 2004

13

A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells

Mark W. Embrey, John S. Wai, Timothy W. Funk, Carl F. Homnick, Debbie S. Perlow, Steven D. Young, Joseph P. Vacca, Daria J. Hazuda, Peter J. Felock, Kara A. Stillmock, Marc V. Witmer, Gregory Moyer, W

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2005

Langue:

english

Fichier:

PDF, 145 KB

english, 2005

14

Conformationally biased P3 amide replacements of β-secretase inhibitors

Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Min-Chi Crouthamel, Beth L. Pietrak, Ming-Tain Lai, M. Katharine Holloway, Sanjeev K. Munshi, Samuel L. Graham, Joseph P. Vacca

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2006

Langue:

english

Fichier:

PDF, 162 KB

english, 2006

15

Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors

John S. Wai, Boyoung Kim, Thorsten E. Fisher, Linghang Zhuang, Mark W. Embrey, Peter D. Williams, Donnette D. Staas, Chris Culberson, Terry A. Lyle, Joseph P. Vacca, Daria J. Hazuda, Peter J. Felock,

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 226 KB

english, 2007

16

8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors

Thorsten E. Fisher, Boyoung Kim, Donnette D. Staas, Terry A. Lyle, Steven D. Young, Joseph P. Vacca, Matthew M. Zrada, Daria J. Hazuda, Peter J. Felock, William A. Schleif, Lori J. Gabryelski, M. Reza

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2007

Langue:

english

Fichier:

PDF, 143 KB

english, 2007

17

Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors

H. Marie Langford, Peter D. Williams, Carl F. Homnick, Joseph P. Vacca, Peter J. Felock, Kara A. Stillmock, Marc V. Witmer, Daria J. Hazuda, Lori J. Gabryelski, William A. Schleif

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 140 KB

english, 2008

18

10-Hydroxy-7,8-dihydropyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: Potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutants

Catherine M. Wiscount, Peter D. Williams, Lekhanh O. Tran, Mark W. Embrey, Thorsten E. Fisher, Vanessa Sherman, Carl F. Homnick, D. Donnette Staas, Terry A. Lyle, John S. Wai, Joseph P. Vacca, ZiQiang

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 164 KB

english, 2008

19

Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase

Jeffrey Y. Melamed, Melissa S. Egbertson, Sandor Varga, Joseph P. Vacca, Greg Moyer, Lori Gabryelski, Peter J. Felock, Kara A. Stillmock, Marc V. Witmer, William Schleif, Daria J. Hazuda, Yvonne Leona

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2008

Langue:

english

Fichier:

PDF, 202 KB

english, 2008

20

Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: Development of novel spiropiperidines

Christopher S. Burgey, Craig M. Potteiger, James Z. Deng, Scott D. Mosser, Christopher A. Salvatore, Sean Yu, Shane Roller, Stefanie A. Kane, Joseph P. Vacca, Theresa M. Williams

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2009

Langue:

english

Fichier:

PDF, 707 KB

english, 2009

21

Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors

Kristen L.G. Jones, M. Katharine Holloway, Hua-Poo Su, Steven S. Carroll, Christine Burlein, Sinoeun Touch, Daniel J. DiStefano, Rosa I. Sanchez, Theresa M. Williams, Joseph P. Vacca, Craig A. Coburn

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 714 KB

english, 2010

22

Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality

Michael R. Wood, Kathy M. Schirripa, June J. Kim, Rodney A. Bednar, John F. Fay, Joseph G. Bruno, Eric L. Moore, Scott D. Mosser, Shane Roller, Christopher A. Salvatore, Joseph P. Vacca, Harold G. Sel

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 719 KB

english, 2010

23

Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffold

Peter D. Williams, Donnette D. Staas, Shankar Venkatraman, H. Marie Loughran, Rowena D. Ruzek, Theresa M. Booth, Terry A. Lyle, John S. Wai, Joseph P. Vacca, Bradley P. Feuston, Linda T. Ecto, Jessica

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2010

Langue:

english

Fichier:

PDF, 320 KB

english, 2010

24

A convergent synthesis of novel conformationally restricted HIV-1 protease inhibitors

B.Moon Kim, James P. Guare, Colleen M. Hanifin, Deborah J. Arford-Bickerstaff, Joseph P. Vacca, Richard G. Ball

Journal:

Tetrahedron Letters

Année:

1994

Langue:

english

Fichier:

PDF, 353 KB

english, 1994

25

Superior methodology for γ-lactone annulation: intramolecular : Alkoxyhydride reduction of conjugated nitriles

Peter T. Lansbury, Joseph P. Vacca

Journal:

Tetrahedron Letters

Année:

1982

Langue:

english

Fichier:

PDF, 245 KB

english, 1982

26

The total synthesis of (±)-myo-inositol-1,3,4-trisphosphate, (±)-myo-inositol-2,4,5-trisphosphate and (±)-myo-inositol-1,3,4,5-tetrakisphosphate

S.Jane deSolms, Joseph P. Vacca, Joel R. Huff

Journal:

Tetrahedron Letters

Année:

1987

Langue:

english

Fichier:

PDF, 201 KB

english, 1987

27

Novel conformationally constrained HIV-1 protease inhibitors: rational design, enzyme inhibition, and X-ray structure of an enzyme-inhibtor complex

B.Moon Kim, Joseph P. Vacca, Paula M.D. Fitzgerald, Paul L. Darke, M.Katharine Holloway, James P. Guare, Colleen M. Hanifin, Deborah J. Arford-Bickerstaff, Joan A. Zugay, Jenny M. Wai, Paul S. Anderso

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1994

Langue:

english

Fichier:

PDF, 2.01 MB

english, 1994

28

Synthesis and evaluation of pyridyl analogs of L-735,524: Potent HIV-1 protease inhibitors

Bruce D. Dorsey, Stacey L. McDaniel, Rhonda B. Levin, Joseph P. Vacca, Paul L. Darke, Joan A. Zuga, Emilio A. Emini, William A. Schleif, Jiunn H. Lin, I-W. Chen, M.Katharine Holloway, Paul S. Anderson

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1994

Langue:

english

Fichier:

PDF, 406 KB

english, 1994

29

L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor

Philip E.J. Sanderson, Dona L. Dyer, Adel M. Naylor-Olsen, Joseph P. Vacca, Steven J. Gardell, S. Dale Lewis, Bobby J. Lucas Jr., Elizabeth A. Lyle, Joseph J. Lynch Jr., Anne M. Mulichak

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1997

Langue:

english

Fichier:

PDF, 237 KB

english, 1997

30

Identification and SAR for a selective, nonpeptidyl thrombin inhibitor

Adel M. Naylor-Olsen, Gerald S. Ponticello, S.Dale Lewis, Anne M. Mulichak, Zhonguo Chen, Charles N. Habecker, Brian T. Phillips, William M. Sanders, Thomas J. Tucker, Jules A. Shafer, Joseph P. Vacca

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1998

Langue:

english

Fichier:

PDF, 382 KB

english, 1998

31

Synthesis, antiviral activity, and bioavailability studies of γ-lactam derived HIV protease inhibitors

Randall W. Hungate, Jenny L. Chen, Ken E. Starbuck, Joseph P. Vacca, Stacey L. McDaniel, Rhonda B. Levin, Bruce D. Dorsey, James P. Guare, M.Katharine Holloway, Willie Whitter, Paul L. Darke, Joan A.

Journal:

Bioorganic & Medicinal Chemistry

Année:

1994

Langue:

english

Fichier:

PDF, 5.38 MB

english, 1994

32

Total synthesis of pseudoguaianolides III. (±)-Aromatin

Peter T. Lansbury, Joseph P. Vacca

Journal:

Année:

1982

Langue:

english

Fichier:

PDF, 577 KB

english, 1982

33

Aromatic P1 replacements for the highly potent HIV-1 protease inhibitor CRIXIVAN®

Craig A. Coburn, Mary Beth Young, Randall W. Hungate, Richard C.A. Isaacs, Joseph P. Vacca, Joel R. Huff

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

1996

Langue:

english

Fichier:

PDF, 164 KB

english, 1996

34

The total synthesis of myo-inositol polyphosphates

Joseph P. Vacca, S.Jane deSolms, Joel R. Huff, David C. Billington, Raymond Baker, Janusz J. Kulagowski, Ian M. Mawer

Journal:

Année:

1989

Langue:

english

Fichier:

PDF, 1.52 MB

english, 1989

35

The structural water of fibrin molecules measured by heat drying and compared with derivations from electron microscopic molecular models

Günter Köppel, Joseph G. Vacca

Journal:

Cell and Tissue Research

Année:

1974

Langue:

english

Fichier:

PDF, 2.14 MB

english, 1974

36

Pancreatic function in cirrhosis of the liver

Guy E. Van Goidsenhoven, Wilbert J. Henke, Joseph B. Vacca, William A. Knight

Journal:

Digestive Diseases and Sciences

Année:

1963

Langue:

english

Fichier:

PDF, 778 KB

english, 1963

37

Identification of a novel RAMP-independent CGRP receptor antagonist

C. Blair Zartman, Ian M. Bell, Steven N. Gallicchio, Samuel L. Graham, Stefanie A. Kane, John J. Mallee, Ruth Z. Rutledge, Christopher A. Salvatore, Joseph P. Vacca, Theresa M. Williams

Journal:

Bioorganic & Medicinal Chemistry Letters

Année:

2011

Langue:

english

Fichier:

PDF, 500 KB

english, 2011

38

Metabolite–P450 Complex Formation by Methylenedioxyphenyl HIV Protease Inhibitors in Rat and Human Liver Microsomes

Masato Chiba, Joy A Nishime, I-Wu Chen, Kari J Vastag, Yousif S Sahly, Byeong Moon Kim, Bruce D Dorsey, Joseph P Vacca, Jiunn H Lin

Journal:

Biochemical Pharmacology

Année:

1998

Langue:

english

Fichier:

PDF, 539 KB

english, 1998

39

Clinically effective HIV-1 protease inhibitors

Joseph P. Vacca, Jon H. Condra

Journal:

Drug Discovery Today

Année:

1997

Langue:

english

Fichier:

PDF, 1.25 MB

english, 1997

40

The human melanoma associated protein melanotransferrin promotes endothelial cell migration and angiogenesis in vivo

Roberta Sala, Wilfred A. Jefferies, Brandie Walker, Joseph Yang, Jacqueline Tiong, S.K. Alex Law, Mariella F. Carlevaro, Eddy Di Marco, Angelo Vacca, Ranieri Cancedda, Fiorella Descalzi Cancedda, Dome

Journal:

European Journal of Cell Biology

Année:

2002

Langue:

english

Fichier:

PDF, 350 KB

english, 2002

41

Design of Novel, Potent, Noncovalent Inhibitors of Thrombin with Nonbasic P-1 Substructures: Rapid Structure−Activity Studies by Solid-Phase Synthesis

Lumma,, William C., Witherup, Keith M., Tucker, Thomas J., Brady, Steven F., Sisko, John T., Naylor-Olsen, Adel M., Lewis, S. Dale, Lucas, Bobby J., Vacca, Joseph P.

Journal:

Journal of Medicinal Chemistry

Année:

1998

Langue:

english

Fichier:

PDF, 83 KB

english, 1998

42

Clinical evaluation of acetyl-digitoxin

Joseph B. Vacca, Joseph M. Schuster, William A. Knight Jr.

Journal:

The American Journal of Cardiology

Année:

1958

Langue:

english

Fichier:

PDF, 569 KB

english, 1958

43

Ebstein's anomaly∗: Complete review of 108 cases

Joseph B. Vacca, Donald W. Bussmann, J.Gerard Mudd

Journal:

The American Journal of Cardiology

Année:

1958

Langue:

english

Fichier:

PDF, 1.11 MB

english, 1958

44

Ebstein's anomaly

Joseph B. Vacca, Donald W. Bussman, J.Gerard Mud

Journal:

The American Journal of Cardiology

Année:

1983

Langue:

english

Fichier:

PDF, 123 KB

english, 1983

45

Serum lipid studies in familial hypercholesterolemic xanthomatosis

Richard C. Powell, Joseph B. Vacca

Journal:

The American Journal of Medicine

Année:

1961

Langue:

english

Fichier:

PDF, 504 KB

english, 1961

46

Discovery and Evaluation of Potent P 1 Aryl Heterocycle-Based Thrombin Inhibitors

Young, Mary Beth, Barrow, James C., Glass, Kristen L., Lundell, George F., Newton, Christina L., Pellicore, Janetta M., Rittle, Kenneth E., Selnick, Harold G., Stauffer, Kenneth J., Vacca, Joseph P.,

Journal:

Journal of Medicinal Chemistry

Année:

2004

Langue:

english

Fichier:

PDF, 350 KB

english, 2004

47

Design and Synthesis of Conformationally Constrained Inhibitors of Non-Nucleoside Reverse Transcriptase

Gomez, Robert, Jolly, Samson J., Williams, Theresa, Vacca, Joseph P., Torrent, Maricel, McGaughey, Georgia, Lai, Ming-Tain, Felock, Peter, Munshi, Vandna, DiStefano, Daniel, Flynn, Jessica, Miller, Mi

Journal:

Journal of Medicinal Chemistry

Année:

2011

Langue:

english

Fichier:

PDF, 2.57 MB

english, 2011

48

Approaches Toward New Alzheimer's Treatments

Vacca, Joseph P.

Journal:

ACS Medicinal Chemistry Letters

Année:

2012

Langue:

english

Fichier:

PDF, 126 KB

english, 2012

49

Design and Synthesis of 8-Hydroxy-[1,6]Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells

Zhuang, Linghang, Wai, John S., Embrey, Mark W., Fisher, Thorsten E., Egbertson, Melissa S., Payne, Linda S., Guare,, James P., Vacca, Joseph P., Hazuda, Daria J., Felock, Peter J., Wolfe, Abigail L.,

Journal:

Journal of Medicinal Chemistry

Année:

2003

Langue:

english

Fichier:

PDF, 80 KB

english, 2003

50

L-735,524: The Design of a Potent and Orally Bioavailable HIV Protease Inhibitor

Dorsey, Bruce D., Levin, Rhonda B., McDaniel, Stacy L., Vacca, Joseph P., Guare, James P., Darke, Paul L., Zugay, Joan A., Emini, Emilio A., Schleif, William A.

Journal:

Journal of Medicinal Chemistry

Année:

1994

Langue:

english

Fichier:

PDF, 2.17 MB

english, 1994